138995-86-5Relevant academic research and scientific papers
Synthesis, in vitro urease inhibitory activity and molecular docking of 3,5-disubstituted thiadiazine-2-thiones
Shah, Muhammad Ishaq Ali,Khan, Rasool,Arfan, Mohammad,Wadood, Abdul,Ghufran, Mehreen
, p. 3073 - 3080 (2019)
A series of 3,5-disubstituted-tetrahydro-thiadiazine-2-thione (1-16) have been synthesized, characterized by elemental analysis, infrared (IR), UV-visible, 1H NMR, 13C NMR, and MS spectroscopic techniques, and screened against jack bean urease. Among 16 compounds, compounds (1), (2), (3), (4), (6), (7), and (9) demonstrated excellent urease inhibitory activity with IC50 values (9.8?±?0.5, 11.0?±?0.6, 16.0?±?1.5, 17.2?±?0.5, 15.4?±?0.5, 19.7?±?0.4, and 15.8?±?0.2μM), respectively, even better than the standard thiourea (IC50?=?21?±?0.01μM). However, compound (8) shows an almost same level of inhibition (IC50?=?22.9?±?0.3μM), as like standard. In this work, we reported for the first time urease inhibitory activity of thiadiazine thiones and its molecular docking studies.
Synthesis and antifungal activities of some new tetrahydro-2H-1,3,5-thiadiazine-2-thiones
Ertan,Ayyildiz,Yulug
, p. 1182 - 1185 (2007/10/02)
A number of new 3-benzyl-5-[α-(substituted)carboxymethyl]-tetrahydro-2H- 1,3,5-thiadiazine-2-thiones has been synthesized as prodrugs by incorporating the amine group of some amino acid into tetrahydro-2H-1,3,5-thiadiazine-2-thione ring. The compounds have been prepared by the reactions of benzylamine with potassium hydroxide, carbon disulphide formaldehyde and various amino acids. The structures of the compounds have been elucidated by UV, IR, 1H-NMR, mass spectra and elementary analysis. The in vitro activity of these compounds against yeast-like fungi (Candida albicans, C. parapsilosis, C. pseudotropicalis, C. stellatoidea) was investigated by tube dilution method. Their minimal inhibitory concentration (MIC) and minimal fungicidal concentration (MFC) values were determined. All the compounds were found to be active between 3.12- 12.5 μg/ml against the four fungi tested.
